OSI-930
Modify Date: 2024-01-21 13:43:29
OSI-930 structure
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Common Name | OSI-930 | ||
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| CAS Number | 728033-96-3 | Molecular Weight | 443.441 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 517.4±50.0 °C at 760 mmHg | |
| Molecular Formula | C22H16F3N3O2S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 266.7±30.1 °C | |
Use of OSI-930OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.IC50 value: 9 nM(VEGFR2); 15 nM(CSF1R); 80 nM (Kit activated) [1]Target: VEGFR2/Kit/CSF1Rin vitro: OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. Moreover, OSI-930 also induces apoptosis in HMC-1 cell line with EC50 of 34 nM [1]. A recent study shows that OSI-930 inactivates purified, recombinant cytochrome P450 (P450) 3A4 with a Ki of 24 μM in a time- and concentration-dependent mode [2].in vivo: OSI-930, administrated at the maximally efficacious dose of 200 mg/kg by oral gavage, exhibits potent antitumor activity in a broad range of preclinical xenograft models including HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models [1]. |
| Name | 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide |
|---|---|
| Synonym | More Synonyms |
| Description | OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.IC50 value: 9 nM(VEGFR2); 15 nM(CSF1R); 80 nM (Kit activated) [1]Target: VEGFR2/Kit/CSF1Rin vitro: OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. Moreover, OSI-930 also induces apoptosis in HMC-1 cell line with EC50 of 34 nM [1]. A recent study shows that OSI-930 inactivates purified, recombinant cytochrome P450 (P450) 3A4 with a Ki of 24 μM in a time- and concentration-dependent mode [2].in vivo: OSI-930, administrated at the maximally efficacious dose of 200 mg/kg by oral gavage, exhibits potent antitumor activity in a broad range of preclinical xenograft models including HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models [1]. |
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| Related Catalog | |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 517.4±50.0 °C at 760 mmHg |
| Molecular Formula | C22H16F3N3O2S |
| Molecular Weight | 443.441 |
| Flash Point | 266.7±30.1 °C |
| Exact Mass | 443.091522 |
| PSA | 91.49000 |
| LogP | 5.10 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Index of Refraction | 1.687 |
| Storage condition | -20℃ |
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OSI-930 CAS#:728033-96-3 |
| Literature: US2004/186124 A1, ; Page/Page column 12 ; |
| Precursor 2 | |
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| DownStream 0 | |
| 3-[(quinolin-4-ylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide |
| N-(4-trifluoromethoxyphenyl) 3-[(quinolin-4-ylmethyl)amino]thiophene-2-carboxamide |
| 3-[(4-Quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide |
| OSI-930 |
| 2-Thiophenecarboxamide, 3-[(4-quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]- |
| S1220_Selleck |